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Cangrelor

Pronunciation

(KAN grel or)

Index Terms

  • Cangrelor Tetrasodium

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Solution Reconstituted, Intravenous:

Kengreal: 50 mg (1 ea)

Brand Names: U.S.

  • Kengreal

Pharmacologic Category

  • Antiplatelet Agent
  • Antiplatelet Agent, Non-thienopyridine

Pharmacology

Cangrelor, a nonthienopyridine adenosine triphosphate analogue, is a direct P2Y12 platelet receptor inhibitor that blocks adenosine diphosphate (ADP)-induced platelet activation and aggregation. Cangrelor binds selectively and reversibly to the P2Y12 receptor, preventing further signaling and platelet activation.

Distribution

Volume of distribution: 3.9 L

Metabolism

Rapidly inactivated in the circulation by dephosphorylation to its primary metabolite, a nucleoside, which has negligible anti-platelet activity

Excretion

Urine (58%); feces (35%)

Onset of Action

Platelet inhibition occurs within 2 minutes

Time to Peak

Within 2 minutes

Duration of Action

Antiplatelet effect is maintained throughout duration of infusion. After discontinuation, platelet function returns to normal within 1 hour

Half-Life Elimination

~3 to 6 minutes

Protein Binding

~97% to 98%

Use: Labeled Indications

Percutaneous coronary intervention (PCI): Adjunct to PCI to reduce the risk of periprocedural myocardial infarction (MI), repeat coronary revascularization, and stent thrombosis in patients who have not been treated with a P2Y12 platelet inhibitor and are not being given a glycoprotein IIb/IIIa inhibitor

Contraindications

Known hypersensitivity (eg, anaphylaxis) to cangrelor or any component of the formulation; significant active bleeding

Dosing: Adult

Percutaneous coronary intervention (PCI): IV: 30 mcg/kg bolus prior to PCI followed immediately by an infusion of 4 mcg/kg/minute continued for at least 2 hours or for the duration of the PCI, whichever is longer.

Transitioning patients to oral P2Y12 antagonist therapy after PCI:

Conversion to clopidogrel: Administer 600 mg of clopidogrel immediately after discontinuing cangrelor infusion. Do not administer clopidogrel prior to cangrelor discontinuation.

Conversion to prasugrel: Administer 60 mg of prasugrel immediately after discontinuing cangrelor infusion. Do not administer prasugrel prior to cangrelor discontinuation.

Conversion to ticagrelor: Administer 180 mg of ticagrelor at any time during cangrelor infusion or immediately after discontinuing cangrelor infusion.

Bridging therapy prior to cardiac surgery (off-label use): IV: 0.75 mcg/kg/min (without a bolus dose) following thienopyridine discontinuation for up to 7 days prior to surgery; discontinue 1 to 6 hours prior to surgical incision (Angiolillo 2012).

Dosing: Geriatric

Refer to adult dosing

Dosing: Renal Impairment

No dosage adjustment necessary

Dosing: Hepatic Impairment

No dosage adjustment necessary

Reconstitution

Reconstitute 50 mg vial by adding 5 mL of Sterile Water for Injection. Swirl gently until dissolved (should be clear and colorless to pale yellow). Avoid vigorous mixing. Allow any foam to settle. Must be diluted prior to administration. Immediately after reconstitution, add the contents of one vial to 250 mL of NS or D5W; mix thoroughly. Resultant concentration of solution for infusion: 200 mcg/mL.

Patients ≥100 kg will require a minimum of 2 bags.

Administration

IV: Vial must be diluted prior to infusion. Administer via a dedicated IV line.

Obtain bolus volume from the prepared bag and administer rapidly over <1 minute via manual IV push or the infusion pump. Ensure the bolus is completely administered before the start of PCI. Start the infusion immediately after administration of the bolus.

Compatibility

Stable in NS, D5W

Storage

Store at controlled room temperature between 20°C and 25°C (68°F and 77°F); excursions are permitted to 15°C to 30°C (59°F and 86°F). Solutions diluted for infusion are stable for up to 12 hours in D5W or 24 hours in NS at room temperature.

Drug Interactions

Agents with Antiplatelet Properties (e.g., P2Y12 inhibitors, NSAIDs, SSRIs, etc.): May enhance the antiplatelet effect of other Agents with Antiplatelet Properties. Monitor therapy

Anticoagulants: Agents with Antiplatelet Properties may enhance the anticoagulant effect of Anticoagulants. Monitor therapy

Apixaban: Antiplatelet Agents (P2Y12 Inhibitors) may enhance the adverse/toxic effect of Apixaban. Specifically, the risk for bleeding may be increased. Management: Carefully consider risks and benefits of this combination and monitor closely; Canadian labeling recommends avoiding prasugrel or ticagrelor. Consider therapy modification

Cephalothin: Agents with Antiplatelet Properties may enhance the adverse/toxic effect of Cephalothin. Specifically, the risk for bleeding may be increased. Monitor therapy

Clopidogrel: Cangrelor may diminish the antiplatelet effect of Clopidogrel. More specifically, while the use of Cangrelor is expected to increase total platelet inhibition in patients who have previously received Clopidogrel, Cangrelor is expected to decrease binding of Clopidogrel metabolites to P2Y12 receptors and thus reduce the extent of irreversible platelet inhibition. Management: Avoid administration of clopidogrel until cangrelor infusion is discontinued. Consider therapy modification

Collagenase (Systemic): Agents with Antiplatelet Properties may enhance the adverse/toxic effect of Collagenase (Systemic). Specifically, the risk of injection site bruising and/or bleeding may be increased. Monitor therapy

Dabigatran Etexilate: Antiplatelet Agents (P2Y12 Inhibitors) may enhance the adverse/toxic effect of Dabigatran Etexilate. Specifically, the risk of bleeding may be increased. Antiplatelet Agents (P2Y12 Inhibitors) may increase the serum concentration of Dabigatran Etexilate. Specifically, clopidogrel may increase dabigatran serum concentrations. Management: Carefully consider risks and benefits of this combination and monitor closely; Canadian labeling recommends avoiding prasugrel or ticagrelor. Consider therapy modification

Dasatinib: May enhance the anticoagulant effect of Agents with Antiplatelet Properties. Monitor therapy

Deoxycholic Acid: Agents with Antiplatelet Properties may enhance the adverse/toxic effect of Deoxycholic Acid. Specifically, the risk for bleeding or bruising in the treatment area may be increased. Monitor therapy

Edoxaban: Antiplatelet Agents (P2Y12 Inhibitors) may enhance the adverse/toxic effect of Edoxaban. Specifically, the risk of bleeding may be increased. Management: Carefully consider the anticipated risks and benefits of this combination. If combined, increased monitoring for bleeding is recommended. Consider therapy modification

Glucosamine: May enhance the antiplatelet effect of Agents with Antiplatelet Properties. Monitor therapy

Herbs (Anticoagulant/Antiplatelet Properties) (eg, Alfalfa, Anise, Bilberry): May enhance the adverse/toxic effect of Agents with Antiplatelet Properties. Bleeding may occur. Consider therapy modification

Ibritumomab: Agents with Antiplatelet Properties may enhance the adverse/toxic effect of Ibritumomab. Both agents may contribute to impaired platelet function and an increased risk of bleeding. Monitor therapy

Ibrutinib: May enhance the adverse/toxic effect of Agents with Antiplatelet Properties. Monitor therapy

Limaprost: May enhance the antiplatelet effect of Agents with Antiplatelet Properties. Monitor therapy

Morphine (Liposomal): May diminish the antiplatelet effect of Antiplatelet Agents (P2Y12 Inhibitors). Morphine (Liposomal) may decrease the serum concentration of Antiplatelet Agents (P2Y12 Inhibitors). Management: Consider alternative anti-ischemic/analgesic therapies (eg, beta-blockers, nitroglycerin) in patients with acute coronary syndromes treated with a P2Y12 inhibitor when possible. The risks associated with other opioids are unknown. Consider therapy modification

Multivitamins/Fluoride (with ADE): May enhance the antiplatelet effect of Agents with Antiplatelet Properties. Monitor therapy

Multivitamins/Minerals (with ADEK, Folate, Iron): May enhance the antiplatelet effect of Agents with Antiplatelet Properties. Monitor therapy

Multivitamins/Minerals (with AE, No Iron): May enhance the antiplatelet effect of Agents with Antiplatelet Properties. Monitor therapy

Obinutuzumab: Agents with Antiplatelet Properties may enhance the adverse/toxic effect of Obinutuzumab. Specifically, the risk of serious bleeding-related events may be increased. Monitor therapy

Omega-3 Fatty Acids: May enhance the antiplatelet effect of Agents with Antiplatelet Properties. Monitor therapy

Pentosan Polysulfate Sodium: May enhance the adverse/toxic effect of Agents with Antiplatelet Properties. Specifically, the risk of bleeding may be increased by concurrent use of these agents. Monitor therapy

Pentoxifylline: May enhance the antiplatelet effect of Agents with Antiplatelet Properties. Monitor therapy

Prasugrel: Cangrelor may diminish the antiplatelet effect of Prasugrel. More specifically, while the use of Cangrelor is expected to increase total platelet inhibition in patients who have previously received Prasugrel, Cangrelor is expected to decrease binding of Prasugrel metabolites to P2Y12 receptors and thus reduce the extent of irreversible platelet inhibition. Management: Avoid administration of prasugrel until cangrelor is discontinued. Consider therapy modification

Prostacyclin Analogues: May enhance the antiplatelet effect of Agents with Antiplatelet Properties. Monitor therapy

Rivaroxaban: Antiplatelet Agents (P2Y12 Inhibitors) may enhance the adverse/toxic effect of Rivaroxaban. Specifically, the risk of bleeding may be increased. Management: Carefully consider risks and benefits of this combination and monitor closely; Canadian labeling recommends avoiding prasugrel or ticagrelor. Consider therapy modification

Salicylates: Agents with Antiplatelet Properties may enhance the adverse/toxic effect of Salicylates. Increased risk of bleeding may result. Monitor therapy

Thrombolytic Agents: Agents with Antiplatelet Properties may enhance the anticoagulant effect of Thrombolytic Agents. Monitor therapy

Tipranavir: May enhance the antiplatelet effect of Agents with Antiplatelet Properties. Monitor therapy

Tositumomab and Iodine I 131 Tositumomab: Agents with Antiplatelet Properties may enhance the adverse/toxic effect of Tositumomab and Iodine I 131 Tositumomab. Specifically, the risk of bleeding-related adverse events may be increased. Monitor therapy

Urokinase: Agents with Antiplatelet Properties may enhance the anticoagulant effect of Urokinase. Avoid combination

Vitamin E (Systemic): May enhance the antiplatelet effect of Agents with Antiplatelet Properties. Monitor therapy

Adverse Reactions

Hematologic & oncologic: Hemorrhage (GUSTO: 16%; TIMI: <1%)

Renal: Renal insufficiency (3%; severe; creatinine clearance <30 mL/minute)

Respiratory: Dyspnea (1%)

<1%, (Limited to important or life threatening): Hypersensitivity reaction

Warnings/Precautions

Concerns related to adverse effects:

• Bleeding: Similar to other P2Y12 antagonists, the use of cangrelor increases the risk of bleeding; however, due to the short elimination half-life, no antiplatelet effect is observed an hour after discontinuation.

• Hypersensitivity: Although rare, serious cases of hypersensitivity (eg, anaphylaxis, anaphylactic shock, bronchospasm, angioedema, stridor) have been reported with cangrelor.

Concurrent drug therapy issues:

• Thienopyridines: If clopidogrel or prasugrel are administered prior to discontinuation of the cangrelor infusion, no antiplatelet effect will occur until the next dose is administered. Therefore, do not administer until after the cangrelor infusion is discontinued.

Monitoring Parameters

Monitor for signs/symptoms of bleeding.

Pregnancy Risk Factor

C

Pregnancy Considerations

Adverse events were observed in some animal reproduction studies.

Patient Education

• Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)

• Have patient report immediately to prescriber signs of bleeding (vomiting blood or vomit that looks like coffee grounds; coughing up blood; hematuria; black, red, or tarry stools; bleeding from the gums; abnormal vaginal bleeding; bruises without a reason or that get bigger; or any severe or persistent bleeding) (HCAHPS).

• Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.

Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for health care professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience and judgment in diagnosing, treating, and advising patients.

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